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Akademický článek

Lead-Discovery of bis-Aromatic Alkynes: A Novel Class of Herbicides

Publikováno v: CHIMIA, Vol 62, Iss 1-2 (2008)

The search for new active molecules with novel modes of action and desirable physical properties is an ongoing endeavour. This publication describes the follow-up chemistry of a biological hit discovered in the screening system of Novartis Crop Prote

Externí odkaz: https://doaj.org/article/5c120d9f6ae7458abd6d1d641fce6442

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Smart design of patient-centric long-acting products: from preclinical to marketed pipeline trends and opportunities

Autor: Céline Bassand, Alessia Villois, Lucas Gianola, Grit Laue, Farshad Ramazani, Bernd Riebesehl, Manuel Sanchez-Felix, Kurt Sedo, Thomas Ullrich, Marieta Duvnjak Romic

Publikováno v: Expert opinion on drug delivery. 19(10)

We see a development in the field of long-acting products to serve patients with chronic diseases by providing benefits in adherence, efficacy, and safety of the treatment. This review investigates features of long-acting products on the market/pipel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6f29eb0d20aed81976f556843041dba
https://pubmed.ncbi.nlm.nih.gov/35877189

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Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360

Autor: Jean-Michel Rondeau, Heinrich Rueeger, Rainer Martin Lueoend, Laura H. Jacobson, Markus Voegtle, Rainer Machauer, Grit Laue, Philipp Holzer, Konstanze Hurth, Siem Jacob Veenstra, Matthias Staufenbiel, Marina Tintelnot-Blomley, Ulf Neumann, Mathias Frederiksen

Publikováno v: Journal of Medicinal Chemistry. 64:4677-4696

Starting from lead compound 4, the 1,4-oxazine headgroup was optimized to improve potency and brain penetration. Focusing at the 6-position of the 5-amino-1,4-oxazine, the insertion of a Me and a CF3 group delivered an excellent pharmacological profi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71a0b16d3116f2d6a82dc5a3b35b580c
https://doi.org/10.1021/acs.jmedchem.0c02143

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Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease

Autor: Ulf Neumann, Rainer Machauer, Markus Voegtle, Marina Tintelnot-Blomley, Konstanze Hurth, Grit Laue, Siem Jacob Veenstra, Rainer Martin Lueoend, Karen Beltz, Jean-Michel Rondeau, Laura H. Jacobson, Heinrich Rueeger

Publikováno v: Journal of medicinal chemistry. 64(20)

After identification of lead compound 6, 5-amino-1,4-oxazine BACE1 inhibitors were optimized in order to improve potency, brain penetration, and metabolic stability. Insertion of a methyl and a trifluoromethyl group at the 6-position of the 5-amino-1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1684187da4ba38d92544db8bc35d7bf0
https://pubmed.ncbi.nlm.nih.gov/34648711

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Discovery of 1 H -pyrazolo[3,4- b ]pyridines as potent dual orexin receptor antagonists (DORAs)

Autor: Arndt Meyer, Murali Chebrolu, Christine E. Gee, Grit Laue, Markus Fendt, Laura H. Jacobson, Sangamesh Badiger, Samuel Hintermann, Chetan Pandit, Simona Cotesta, Claudia Betschart, Daniel Hoyer, Vinod D. Chaudhari, Dirk Behnke, Trixie Wagner

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:5555-5560

Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochem

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::683f840d5741ac67440ee89e98efc728
https://doi.org/10.1016/j.bmcl.2015.10.055

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Communication between plants: induced resistance in wild tobacco plants following clipping of neighboring sagebrush

Autor: K. J. Baxter, Grit Laue, Ian T. Baldwin, Richard Karban, Gary W. Felton

Publikováno v: Scopus-Elsevier

The possibility of communication between plants was proposed nearly 20 years ago, although previous demonstrations have suffered from methodological problems and have not been widely accepted. Here we report the first rigorous, experimental evidence

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4a3d6a4260337bc7aec213af0bca865
https://pubmed.ncbi.nlm.nih.gov/28308223

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Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia

Autor: Chetan Pandit, Christine E. Gee, Daniel Hoyer, Vinod D. Chaudhari, Grit Laue, Juergen Wagner, Laura H. Jacobson, Dirk Behnke, Claudia Betschart, Simona Cotesta, Sangamesh Badiger, Samuel Hintermann, Markus Fendt, Silvio Ofner

Publikováno v: Journal of Medicinal Chemistry. 56:7590-7607

Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clinical trials in volunteers and primary insomnia patients. The r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48dc21e46c9f923dccf5394833956e52
https://doi.org/10.1021/jm4007627

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Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists

Autor: Ivo Vranesic, Peter Ertl, Manuel Koller, Grit Laue, Dirk Behnke, David Orain, Sandrine Desrayaud, David Carcache

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:6454-6459

1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic scaffold allowed to improve the physico-chemical parameters for optimization of the aqueous

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fc51fe950ab99a627e4927771bfbf5e
https://doi.org/10.1016/j.bmcl.2012.08.053

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